| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| Targets |
Thozalinone induces the release of norepinephrine and dopamine in the brain. This mechanism is similar to that of its analogues pemoline and aminorex. By modulating dopaminergic and noradrenergic activity, it produces psychostimulant effects that may enhance mood and alleviate symptoms of depression and fatigue. It is also an antidepressant with activity against tetrabenazine-induced depression.
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|---|---|
| ln Vitro |
Thozalinone is a psychostimulant agent that induces the release of norepinephrine and dopamine. In ICR male mice, Thozalinone (100 mg/kg, ip) appears to provide the best prediction for the psychostimulant-inducing potencies among DL-DOPA, apomorphine, and amphetamine. It has unique properties that distinguish it from sympathomimetic amines.
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| ln Vivo |
In ICR male mice, Thozalinone (100 mg/kg, ip) appears to provide the best prediction for the psychostimulant-inducing potencies among DL-DOPA, apomorphine, and amphetamine. This suggests that it has a distinct pharmacological profile compared to other psychostimulants. Its activity against tetrabenazine-induced depression has also been demonstrated in animal models.
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| Enzyme Assay |
In vitro assays for Thozalinone are not well-documented. Its mechanism of action is primarily studied in vivo through behavioral and neurochemical analyses. However, its effects on neurotransmitter release can be studied in vitro using synaptosomal preparations or cell cultures expressing dopamine and norepinephrine transporters, measuring the release of radiolabeled neurotransmitters.
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| Cell Assay |
In vitro cellular assays for Thozalinone are limited. Its psychostimulant effects are primarily studied in vivo. However, its effects on neuronal cells can be assessed by measuring dopamine and norepinephrine release in cultured neurons or cell lines. Cytotoxicity and cell viability assays can also be performed to evaluate its safety profile in various cell types.
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| Animal Protocol |
In vivo animal models for Thozalinone are used to assess its psychostimulant and antidepressant effects. The tetrabenazine-induced depression model in rodents is used to evaluate its antidepressant activity. The ICR male mouse model is used to predict its psychostimulant-inducing potencies. Other models, such as the forced swim test or tail suspension test, may also be used.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Thozalinone are limited. As a psychostimulant, it is expected to be well-absorbed after oral administration and to cross the blood-brain barrier to exert its central effects. It is likely metabolized in the liver, and its metabolites are excreted in urine. Its half-life and bioavailability are not well-characterized in the literature.
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| Toxicity/Toxicokinetics |
The toxicological profile of Thozalinone is not extensively documented. As a psychostimulant, it may cause side effects such as insomnia, anxiety, palpitations, and increased blood pressure. Its potential for abuse and dependence is a concern, similar to other stimulants. Long-term use may lead to tolerance and withdrawal symptoms.
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| Additional Infomation |
Thozalinone is a synthetic psychostimulant that induces the release of norepinephrine and dopamine. It has been investigated as an antidepressant and for the treatment of narcolepsy and ADHD. It is also known as Stimsen and was developed in the 1960s. It has been used as an antidepressant in Europe and trialed as an anorectic.
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| Molecular Formula |
C11H12N2O2
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|---|---|
| Molecular Weight |
204.22
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| Exact Mass |
204.09
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| CAS # |
655-05-0
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| PubChem CID |
12602
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| Appearance |
White to off-white solid powder
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| Density |
1.19g/cm3
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| Boiling Point |
294.8ºC at 760 mmHg
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| Melting Point |
134.5ºC
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| Flash Point |
132.1ºC
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| Index of Refraction |
1.584
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| LogP |
0.637
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
280
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C1=NC(=O)C(C2C=CC=CC=2)O1)C
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| InChi Key |
JJSHYECKYLDYAR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N2O2/c1-13(2)11-12-10(14)9(15-11)8-6-4-3-5-7-8/h3-7,9H,1-2H3
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| Chemical Name |
2-(dimethylamino)-5-phenyl-1,3-oxazol-4-one
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| Synonyms |
Stimsen; Tozalinone; Thozalinone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8967 mL | 24.4834 mL | 48.9668 mL | |
| 5 mM | 0.9793 mL | 4.8967 mL | 9.7934 mL | |
| 10 mM | 0.4897 mL | 2.4483 mL | 4.8967 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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